Synthesis and Cav2.2 Binding Data for Non-Peptide Mimetics of ω-Conotoxin GVIA based on a 5-Amino-Anthranilamide Core

Article

<< Previous

Next >>

Contents Vol 61(1)

doi:10.1071/CH07327

Synthesis and Ca_v2.2 Binding Data for Non-Peptide Mimetics of ω-Conotoxin GVIA based on a 5-Amino-Anthranilamide Core

Peter J. Duggan ^A, Jonathan M. Faber ^B, Janease E. Graham ^A ^B, Richard J. Lewis ^C, Natalie G. Lumsden ^C, Kellie L. Tuck ^B ^D

^A CSIRO, Molecular and Health Technologies, Bag 10, Clayton South VIC 3169, Australia.
^B School of Chemisty, Monash University, Clayton VIC 3800, Australia.
^C Institute for Molecular Bioscience, The University of Queensland, St Lucia, QLD 4072, Australia.
^D Corresponding author. Email: kellie.tuck@sci.monash.edu.au





	PDF (236 KB) $25



	Export Citation

Print

Australian Journal of Chemistry 61(1) 11–15 http://dx.doi.org/10.1071/CH07327
Submitted: 13 September 2007 Accepted: 29 November 2007 Published online: 18 January 2008

Abstract

A simple and efficient method has been developed for the synthesis of two anthranilamide-based non-peptide mimetics of ω-conotoxin GVIA. These anthranilamide derivatives aim to mimic the K2, R17, and Y13 residues of the peptide. The synthetic route described enables the rapid synthesis of anthranilamide analogues with identical alkyl chain lengths. The target compounds show affinity to rat N-type voltage gated calcium channels (Ca_v2.2) with EC₅₀ values of 42 and 75 μM.